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    Antineoplastic conjugates of transferrin, albumin and polyethylene glycol
    3.
    发明授权
    Antineoplastic conjugates of transferrin, albumin and polyethylene glycol 有权
    转铁蛋白，白蛋白和聚乙二醇的抗肿瘤缀合物

    公开(公告)号：US06310039B1

    公开(公告)日：2001-10-30

    申请号：US09254598

    申请日：1999-05-21

    申请人： Felix Kratz

    发明人： Felix Kratz

    IPC分类号： A61K3838

    CPC分类号： C07K14/79 ,  A61K38/00 ,  A61K47/62 ,  A61K47/643 ,  A61K47/644 ,  A61K47/65 ,  C07K14/76

    摘要： Conjugates of transferrin, albumin and polyethylence glycol consisting of native or thiolated transferrin or albumin or of polyethylene glycol (MW between approximately 5,000 and 20,0000) with at least one HS—, HO— or H2N group and cytostatic compounds derived through maleinimide or N-hydroxysuccinimide ester compounds, such as doxorubicin, daunorubicin, epirubicin, idarubicin, mitoxandrone, chloroambucil, melphalan, 5-fluorouracyl, 5′-desoxy-5-fluorouridine, thioguanine, methotrexate, paclitaxel, docetaxel, topotecan, 9-aminocamptothecin, etoposide, teniposide, mitopodoside, vinblastine, vincristine, vindesine, vinorelbine or a compound of general formula A, B, C or D, where n=0-6, X=—NH2, —OH, —COOH, —O—CO—R—COR*, —NH—CO—R—COR*, where R is an aliphatic carbon chain with 1-6 carbon atoms or a substituted or unsubstituted phenylene group and R* H, phenyl, alkyl with 1-6 carbon atoms.

    摘要翻译： 由天然或硫醇化转铁蛋白或白蛋白或聚乙二醇（约5,000至20,0000的MW）与至少一种HS-，HO-或H2N基团组成的转铁蛋白，白蛋白和聚乙二醇的结合物和通过马来酰亚胺或N 羟基琥珀酰亚胺酯化合物，如多柔比星，柔红霉素，表柔比星，伊达比星，米托蒽醌，氯氮芥，美法仑，5-氟尿嘧啶，5'-脱氧-5-氟尿苷，硫鸟嘌呤，甲氨蝶呤，紫杉醇，多西他赛，托泊替康，9-氨基喜树碱，依托泊苷， 替尼泊苷，mitopodoside，长春花碱，长春新碱，长春地辛，长春瑞滨或通式A，B，C或D的化合物，其中n = 0-6，X = -NH2，-OH，-COOH，-O-CO-R- COR *，-NH-CO-R-COR *，其中R是具有1-6个碳原子的脂族碳链或取代或未取代的亚苯基，R * H，苯基，具有1-6个碳原子的烷基。

    Process for producing an injectable medicament preparation
    7.
    发明授权
    Process for producing an injectable medicament preparation 有权
    生产可注射药物制剂的方法

    公开(公告)号：US08846602B2

    公开(公告)日：2014-09-30

    申请号：US13414316

    申请日：2012-03-07

    申请人： Felix Kratz

    发明人： Felix Kratz

    IPC分类号： A61K51/04 ,  A61P35/00 ,  A61K47/48

    CPC分类号： A61K31/704 ,  A61K9/0019 ,  A61K47/545 ,  A61K47/643 ,  A61K47/65

    摘要： The invention relates to a method for producing injectable medicament preparations containing a therapeutically and/or diagnostically effective substance which is comprised of an active agent, of a spacer molecule and of at least one protein-binding molecule. After being brought into contact with the body, said therapeutically and/or diagnostically effective substance covalently bonds to the body fluid constituents or tissue constituents via the protein-binding molecule, thus providing a form of transport of the active agent that an be hydrolytically or enzymatically cleaved, according to pH, in the body while releasing the active agent.

    摘要翻译： 本发明涉及一种用于制备含有治疗和/或诊断有效物质的可注射药物制剂的方法，其由活性剂，间隔分子和至少一种蛋白质结合分子组成。 在与身体接触后，所述治疗和/或诊断有效物质通过蛋白质结合分子共价键合到体液成分或组织成分，从而提供水解或酶促活性剂的运输形式 根据pH，在释放活性剂的同时在体内裂解。

    Prodrugs
    10.
    发明授权
    Prodrugs 有权
    前药

    公开(公告)号：US08642555B2

    公开(公告)日：2014-02-04

    申请号：US13255812

    申请日：2010-03-09

    申请人： Felix Kratz ,  Andre Warnecke ,  Bakheet Elsadek

    发明人： Felix Kratz ,  Andre Warnecke ,  Bakheet Elsadek

    IPC分类号： A61K38/08

    CPC分类号： C07K5/1013 ,  A61K47/65 ,  C07K5/06069 ,  C07K7/06

    摘要： The present invention relates to a prodrug comprising at least one cytostatic agent, wherein said prodrug is cleavable by prostate-specific antigen (PSA), a process for preparing said prodrug and a pharmaceutical composition containing said prodrug in a pharmaceutically effective amount, for use in the treatment of cancer.

    摘要翻译： 本发明涉及包含至少一种细胞生长抑制剂的前体药物，其中所述前体药物可由前列腺特异性抗原（PSA）切割，制备所述前体药物的方法和药物组合物，所述药物组合物含有药学有效量的所述前体药物， 治疗癌症。